ADU-S100 ammonium salt

SKU: orb1940832

Description

ADU-S100 ammonium salt is an activator of stimulator of interferon genes (STING). ADU-S100 ammonium salt leads to potent and systemic tumor regression and immunity.(In Vitro):ADU-S100 ammonium salt induces the highest expression of IFN-β and the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1 on a molar equivalent basis, as compared to endogenous ML cGAMP and the TLR3 agonist poly I:C. ADU-S100 ammonium salt is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage. ADU-S100 ammonium salt induces significantly higher levels of IFN-α compared to ML cGAMP.(In Vivo):IT injection of ADU-S100 ammonium salt into one tumor in BALB/c mice bearing bilateral CT26 or 4T1 tumors also demonstrated significant regression of the contralateral, untreated tumor. IT injection with ADU-S100 ammonium salt eradicates multiple tumor types and primes an effective systemic CD8+ T cell immune response that significantly inhibits the growth of distal, untreated lesions.

Images & Validation

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Key Properties

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CAS Number	1638750-96-5
MW	724.6
Purity	>98% (HPLC)
Formula	C₂₀H₃₀N₁₂O₁₀P₂S₂
SMILES	[NH4+].[NH4+].[H]C12COP([S-])(=O)OC3C(COP([S-])(=O)OC([H])(C1O)C(O2)n1cnc2c(N)ncnc12)OC(C3O)n1cnc2c(N)ncnc12
Target	STING
Solubility	In Vitro: H2O : 100 mg/mL (138.01 mM)

Bioactivity

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In Vivo

ADU-S100 shows higher anti-tumor control than the endogenous ML cGAMP. A dose response of the ADU-S100 compound is performed in B16 tumor-bearing mice, which identifies an optimal antitumor dose level that also elicites maximum tumor antigen-specific CD8+ T cell responses, and improves long-term survival to 50%.

In Vitro

ADU-S100 ammonium salt has several features that improve both stability and lipophilicity, promoting significantly increased STING signaling as compared to endogenous and pathogen-derived cyclic dinucleotides (CDNs). ADU-S100 shows enhanced type I IFN production over CDA in THP-1 human monocytes. In contrast, the dithio, mixed-linkage cyclic dinucleotide (CDN) derivatives (ML RR-CDA, ML RR-S2 CDG, and ML RR-S2 cGAMP) potently activate all five hSTING alleles, including the refractory hSTINGREF and hSTINGQ alleles. ADU-S100 induces the highest expression of IFN-β and the pro-inflammatory cytokines TNF-α, IL-6, and MCP-1 on a molar equivalent basis, as compared to endogenous ML cGAMP and the TLR3 agonist poly I: C. ADU-S100 is also found to induce aggregation of STING and induce phosphorylation of TBK1 and IRF3 in mouse bone marrow macrophage (BMM). ADU-S100 induces significantly higher levels of IFN-α when compared to ML cGAMP.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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MIW815 ammonium salt | ML RR-S2 CDA ammonium salt

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STING

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